Detalles de la búsqueda
1.
From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell
; 184(24): 5886-5901.e22, 2021 11 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-34822784
2.
Dynamic extracellular vestibule of human SERT: Unveiling druggable potential with high-affinity allosteric inhibitors.
Proc Natl Acad Sci U S A
; 120(41): e2304089120, 2023 10 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-37792512
3.
Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain-a Game Changing Parameter for CNS Drug Discovery and Development.
Pharm Res
; 39(7): 1321-1341, 2022 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-35411506
4.
Characterisation of intravenous pharmacokinetics in Göttingen minipig and clearance prediction using established in vitro to in vivo extrapolation methodologies.
Xenobiotica
; 52(6): 591-607, 2022 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-36000364
5.
Systemic administration of ivabradine, a hyperpolarization-activated cyclic nucleotide-gated channel inhibitor, blocks spontaneous absence seizures.
Epilepsia
; 62(7): 1729-1743, 2021 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-34018186
6.
Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.
Mol Pharmacol
; 93(6): 645-656, 2018 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-29695609
7.
Asc-1 Transporter Regulation of Synaptic Activity via the Tonic Release of d-Serine in the Forebrain.
Cereb Cortex
; 27(2): 1573-1587, 2017 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26796213
8.
Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N-(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT2A Receptor Agonist.
J Pharmacol Exp Ther
; 361(3): 441-453, 2017 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-28360333
9.
Lack of Exposure in a First-in-Man Study Due to Aldehyde Oxidase Metabolism: Investigated by Use of 14C-microdose, Humanized Mice, Monkey Pharmacokinetics, and In Vitro Methods.
Drug Metab Dispos
; 45(1): 68-75, 2017 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27737930
10.
Characterization of [11C]Lu AE92686 as a PET radioligand for phosphodiesterase 10A in the nonhuman primate brain.
Eur J Nucl Med Mol Imaging
; 44(2): 308-320, 2017 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-27817159
11.
The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin.
Bioorg Med Chem Lett
; 27(11): 2629-2633, 2017 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28462834
12.
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).
Mol Pharmacol
; 88(2): 401-20, 2015 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-26056160
13.
In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1.
J Pharmacol Exp Ther
; 354(2): 166-74, 2015 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-25986445
14.
Brexpiprazole Alters Monoaminergic Systems following Repeated Administration: an in Vivo Electrophysiological Study.
Int J Neuropsychopharmacol
; 19(3): pyv111, 2015 Oct 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26428352
15.
Brexpiprazole II: antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator.
J Pharmacol Exp Ther
; 350(3): 605-14, 2014 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-24947464
16.
Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator.
J Pharmacol Exp Ther
; 350(3): 589-604, 2014 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-24947465
17.
Correlating the metabolic stability of psychedelic 5-HT2A agonists with anecdotal reports of human oral bioavailability.
Neurochem Res
; 39(10): 2018-23, 2014 Oct.
Artículo
en Inglés
| MEDLINE | ID: mdl-24519542
18.
Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs.
Neurochem Res
; 39(10): 1964-79, 2014 Oct.
Artículo
en Inglés
| MEDLINE | ID: mdl-24682739
19.
Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration.
Bioorg Med Chem Lett
; 24(1): 288-93, 2014 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-24291041
20.
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
Bioorg Med Chem Lett
; 24(1): 177-80, 2014 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-24355129